scholarly journals DEVELOPMENT OF SUSTAINED RELEASE ALOGLIPTIN TABLETS USING A MULTIPARTICULATES SYSTEM MADE OF BENTONITE

Author(s):  
RASHAD M. KAOUD ◽  
ALHAMZA HOSHI KHALAF ◽  
JAMAL ALYOUSSEF ALKRAD

Objective: This study was designed to evaluate the use of bentonite in the formulation of sustained-release tablets containing alogliptin benzoate after granulation. Methods: Bentonite was used for preparing tablets after granulation. The prepared tablets were tested for their pharmacopeial requirements. Further, a high-performance liquid chromatography (HPLC) method was developed to assess the release pattern of alogliptin from the tablets. Besides, differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and powder X-ray diffraction (XRD) were used for evaluating the compatibility the drugs and bentonite. Finally, the release from the tablets was tested using the paddle apparatus. Results: The FTIR and DSC did not show any interaction between the drug and the excipient in contrast to the powder-XRD pattern, which showed a shift for montmorillonite crystal peak. This shift was interpreted by increasing in the spacing of the crystalline structure of montmorillonite. However, the results of pharmacopeial tests showed that the prepared tablets comply with the compendial requirements, In addition, the release profiles of these tablets with aid of hydroxypropyl methylcellulose (HPMC) as a binder revealed a sustained release of alogliptin. Furthermore, the fitting of release data showed that the release from these tablets followed Fickian diffusion that alogliptin released by diffusion from bentonite gel matrix. Conclusion: Bentonite was successfully used for producing sustained-release tablets of alogliptin. However, maintaining the crystal structure of montmorillonite was essential for building the gel structure of bentonite and releasing the drug in a controlled manner.

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Xiaojun Shang ◽  
Suying Ma ◽  
Zheshen Li

A rapid, sensitive, and reproducible reverse phase high performance liquid chromatographic (RP-HPLC) method with UV detector for the determination of nimodipine in sustained release tablets was developed. The method involved using a SinoChoom ODS-BP C18reversed phase column (5 μm, 4.6 mm × 200 mm) and mobile phase consisting of methanol-acetonitrile-water (35 : 38 : 27, v/v). The flow rate is 1.0 mL/min, the UV detector was operated at 237 nm, and the column was maintained at 25°C. The method was validated according to official compendia guidelines. The calibration curve of nimodipine for RP-HPLC method was linear over the range of 10–100 μg/mL. The retention time was found at 7.50 min for nimodipine. The variation for interday and intraday assay was found to be less than 0.72%. The proposed RP-HPLC was proved to be suitable for the determination of nimodipine in sustained release tablets.


2008 ◽  
Vol 5 (2) ◽  
pp. 316-322 ◽  
Author(s):  
Dimple Chopra ◽  
Vivek Ranjan Sinha ◽  
Manjeet Singh

Differential scanning calorimetry (DSC) is a rapid and convenient and conclusive method of screening drug-polymer blend during preformulation studies as it allows polymer incompatibility to be established instantaneously. Various batches of matrix tablets of ketorolac tromethamine (KTM) with a series of compatible polymers were prepared. Batches of tablets which gave desired sustained release profile were subjected to stability testing according to ICH guidelines. The analysis for drug content was done using high performance liquid chromatography (HPLC) method. The results revealed that there was no statistically significant change in drug content after storage of matrix tablets at elevated temperature of 40°C and 75% relative humidity. From our study we conclude that with careful selection of different polymers and their combinations, a stable sustained release oral dosage form of ketorolac tromethamine can be achieved.


Polymers ◽  
2021 ◽  
Vol 13 (16) ◽  
pp. 2813
Author(s):  
Víctor Guarnizo-Herrero ◽  
Carlos Torrado-Salmerón ◽  
Norma Sofía Torres Pabón ◽  
Guillermo Torrado Durán ◽  
Javier Morales ◽  
...  

This study investigated the combination of different proportions of cationic chitosan and anionic carboxymethyl cellulose (CMC) for the development of polyelectrolyte complexes to be used as a carrier in a sustained-release system. Analysis via scanning electron microscopy (SEM) Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) confirmed ionic interactions occur between the chitosan and carboxymethyl cellulose chains, which increases drug entrapment. The results of the dissolution study in acetate buffer (pH 4.2) showed significant increases in the kinetic profiles of clarithromycin for low proportions of chitosan/carboxymethyl cellulose tablets, while the tablets containing only chitosan had high relaxation of chitosan chains and disintegrated rapidly. The Korsmeyer–Peppas kinetic model for the different interpolymer complexes demonstrated that the clarithromycin transport mechanism was controlled by Fickian diffusion. These results suggest that the matrix tablets with different proportions of chitosan/carboxymethyl cellulose enhanced the ionic interaction and enabled the prolonged release of clarithromycin.


2020 ◽  
Vol 16 (7) ◽  
pp. 950-959
Author(s):  
Yu Li ◽  
Xiangwen Kong ◽  
Fan Hu

Background: Clarithromycin is widely used for infections of helicobacter pylori. Clarithromycin belongs to polymorphic drug. Crystalline state changes of clarithromycin in sustained release tablets were found. Objective: The aim of this study was to find the influential factor of the crystal transition of clarithromycin in preparation process of sustained-release tablets and to investigate the possible interactions between the clarithromycin and pharmaceutical excipients. Methods and Results: The crystal transition of active pharmaceuticals ingredients from form II to form I in portion in clarithromycin sustained release tablets were confirmed by x-ray powder diffraction. The techniques including differential scanning calorimetry and infrared spectroscopy, x-ray powder diffraction were used for assessing the compatibility between clarithromycin and several excipients as magnesium stearate, lactose, sodium carboxymethyl cellulose, polyvinyl-pyrrolidone K-30 and microcrystalline cellulose. All of these methods showed compatibilities between clarithromycin and the selected excipients. Alcohol prescription simulation was also done, which showed incompatibility between clarithromycin and concentration alcohol. Conclusion: It was confirmed that the reason for the incompatibility of clarithromycin with high concentration of alcohol was crystal transition.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1008 ◽  
Author(s):  
Qilei Yang ◽  
Chang Zu ◽  
Wengang Li ◽  
Weiwei Wu ◽  
Yunlong Ge ◽  
...  

Paclitaxel (PTX) is a poor water-soluble antineoplastic drug with significant antitumor activity. However, its low bioavailability is a major obstacle for its biomedical applications. Thus, this experiment is designed to prepare PTX crystal powders through an antisolvent precipitation process using 1-hexyl-3-methylimidazolium bromide (HMImBr) as solvent and water as an antisolvent. The factors influencing saturation solubility of PTX crystal powders in water in water were optimized using a single-factor design. The optimum conditions for the antisolvent precipitation process were as follows: 50 mg/mL concentration of the PTX solution, 25 °C temperature, and 1:7 solvent-to-antisolvent ratio. The PTX crystal powders were characterized via scanning electron microscopy, Fourier transform infrared spectroscopy, high-performance liquid chromatography–mass spectrometry, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Raman spectroscopy, solid-state nuclear magnetic resonance, and dissolution and oral bioavailability studies. Results showed that the chemical structure of PTX crystal powders were unchanged; however, precipitation of the crystalline structure changed. The dissolution test showed that the dissolution rate and solubility of PTX crystal powders were nearly 3.21-folds higher compared to raw PTX in water, and 1.27 times higher in artificial gastric juice. Meanwhile, the bioavailability of PTX crystal increased 10.88 times than raw PTX. These results suggested that PTX crystal powders might have potential value to become a new oral PTX formulation with high bioavailability.


2013 ◽  
Vol 49 (3) ◽  
pp. 571-578 ◽  
Author(s):  
Payal Hasmukhlal Patil ◽  
Veena Sailendra Belgamwar ◽  
Pratibha Ramratan Patil ◽  
Sanjay Javerilal Surana

The objective of the present work was to enhance the solubility and dissolution rate of the drug raloxifene HCl (RLX), which is poorly soluble in water. The solubility of RLX was observed to increase with increasing concentration of hydroxypropyl methylcellulose (HPMC E5 LV). The optimized ratio for preparing a solid dispersion (SD) of RLX with HPMC E5 LV using the microwave-induced fusion method was 1:5 w/w. Microwave energy was used to prepare SDs. HPMC E5 LV was used as a hydrophilic carrier to enhance the solubility and dissolution rate of RLX. After microwave treatment, the drug and hydrophilic polymer are fused together, and the drug is converted from the crystalline form into an amorphous form. This was confirmed through scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies. These results suggested that the microwave method is a simple and efficient method of preparing SDs. The solubility and dissolution rate of the SDs were increased significantly compared with pure RLX due to the surfactant and wetting properties of HPMC E5 LV and the formation of molecular dispersions of the drug in HPMC E5 LV. It was concluded that the solubility and dissolution rate of RLX are increased significantly when an SD of the drug is prepared using the microwave-induced fusion method.


2021 ◽  
Vol 14 (1) ◽  
pp. 41-48
Author(s):  
Larisa Cimpoaie ◽  
◽  
Luca Liviu Rus ◽  
Rareș Iuliu Iovanov ◽  
◽  
...  

Objectives. The aim of this study was to investigate the influence of formulation factors on in vitro release of ketoprofen from sustained release inert matrix tablets. Materials and methods. Laboratory scale, Ketoprofen sustained release inert matrix tablets were manufactured using Kollidon® SR as matrix formator, by direct tableting of powder blends. The influence of the formulation factors (X1 – matrix formator excipient and X2 – diluent type) on in vitro release of ketoprofen from sustained release tablets was studied by using a full factorial 23 experimental plan. Outcomes. Pharmacotechnical characterization of manufactured laboratory scale batches was performed and all 12 batches fulfilled European Pharmacopeia requests. In vitro release showed a sustained release profile in all cases. Variance analysis (ANOVA) showed a good correlation between experimental conditions and answers. In vitro release testing was performed in phosphate buffer pH = 7.4. Percentage release was determined spectrophotometrically at 258 nm. A decrease in the rate of in vitro release was registered, up to 4 h and 6 h when lactose DC and mannitol DC were used as diluents, respectively. Isomalt DC has increased the rate of in vitro release up to 6 h. Conclusions. In vitro release data, corresponding to formulation N1 shoed a good fitting with Weitbull, Korshmeyer-Peppas and Higuchi models while in vitro release data corresponding to formulation N8 presented a good fitting with Weitbull and Korsmeyer-Peppas. In case of formulations N1 and N8 a non-Fickian diff usion mechanism seems to be involved in drug release from the matrix tablets.


2015 ◽  
Vol 817 ◽  
pp. 96-103
Author(s):  
Wei Ping Fang ◽  
Yao Yong Yi ◽  
Feng Mei Liu ◽  
Zheng Lin Liu ◽  
Zhen Hua Deng

A silver free amorphous Cu-35Ti-12Ni active brazing alloy was successfully prepared in this work. The crystallinity, microstructure, and chemical composition were characterized with X-ray diffraction (XRD), scanning electron microscope (SEM), and energy-dispersive spectrometry (EDS), respectively. A typical characteristic peak of amorphous material was observed in the XRD pattern. The microstructures and chemical compositions of the silver free amorphous alloy were uniform. Differential scanning calorimetry (DSC) result shows that the amorphous silver free brazing alloy has higher melting temperature than commercial silver brazing alloy (Ag-26.5Cu-1.5Ti). Wetting contact angle and spreading area on Si3N4 ceramic substrate were used to evaluate the wetting ability of brazing alloy. The wetting angle was smaller than 5o, and the spreading area was 141.6 mm2 at 1100°C. The bending strength of silver free brazing alloy/Si3N4 was also carried out. The mechanical test shows that the amorphous Cu-35Ti-12Ni/Si3N4 has higher joint strength (304.7MPa) than the crystal Cu-35Ti-12Ni/Si3N4 (294.7MPa) at room temperature.


2020 ◽  
pp. 096739112090447
Author(s):  
O Sreekanth Reddy ◽  
MCS Subha ◽  
T Jithendra ◽  
C Madhavi ◽  
K Chowdoji Rao

This article reports the fabrication of pH-sensitive microbeads from sodium alginate (SA) and modified karaya gum (KG). KG was modified by graft copolymerization using 2-hydroxyethyl methacrylate (2-HEMA) through in situ free radical polymerization reaction. The graft copolymer was blended with SA to develop microbeads by a simple ionotropic gelation technique. The microbeads were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. The effect of %HEMA and polymer blend ratio on the swelling capacity was investigated. Drug release kinetics of the microbeads was investigated under both pH 7.4 and pH 1.2 at 37°C. The drug release kinetics was analyzed by evaluating the release data using different kinetic models.


2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Lan Chen ◽  
Bo Bai

Phosphotungstic acid (HPW)-impregnated yeast hybrid microspheres were prepared by impregnation-adsorption technique through tuning pH of the aqueous yeast suspensions. The obtained products were characterized by field emission scanning electron microscopy (FE-SEM), energy dispersive spectrometry (EDS), X-ray diffraction (XRD), thermogravimetry-differential scanning calorimetry (TG-DSC), and ultraviolet-visible spectrophotometry (UV-Vis), respectively. FE-SEM and EDS ascertain that the HPW has been effectively introduced onto the surface of yeast, and the resulting samples retain ellipsoid shape, with the uniform size (length 4.5 ± 0.2 μm, width 3.0 ± 0.3 μm) and good monodispersion. XRD pattern indicates that the main crystal structure of as-synthesized HPW@yeast microsphere is Keggin structure. TG-DTA states that the HPW in composites has better thermal stability than pure HPW. Fourier transform infrared spectroscopy (FT-IR) elucidates that the functional groups or chemical bonds inherited from the pristine yeast cell were critical to the assembling of the composites. UV-Vis shows that the obtained samples have a good responding to UV light. The settling ability indicates that the hybrid microspheres possess an excellent suspension performance. In the test of catalytic activity, the HPW@yeast microsphere exhibits a high photocatalytic activity for the decoloration of Methylene blue and Congo red dye aqueous solutions, and there are a few activity losses after four cycles of uses.


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